D5B
Based on 1 Customer Validation
D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC50 of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.94%
- 分子式: C58H66N2O12
- 分子量:983.15
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
EC50: 5.4 μM (PD-L1 in 4T1 tumor cells)[1]
EC50: 6.2 μM (PD-L1 in B16-F10 tumor cells)[1]
D5B (0-10 μM; 24 h) can degrade PD-L1 in 4T1 and B16-F10 tumor cells with EC50 of 5.4 μM and 6.2 μM, respectively[1].
D5B (0-5 μM; 48 h) significantly decreases the PD-L1 abundance on cell membrane surface in IFN-γ treated and azide-labeled 4T1 and B16-F10 tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IFN-γ treated and azide-labeled 4T1 and B16-F10 tumor cells
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Concentration:0, 1.25, 2.5 and 5.0 μM
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Incubation Time:48 h
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Result:Significantly reduced the level of PD-L1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4T1 tumor-bearing mice with radiotherapy[1]
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Dosage:5 mg/kg (D5B is in the form of PCPGd@D5B nanoparticles)
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Administration:Intraperitoneal injection (i.p.); Single dose
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Result:Completely eradicated 50% of the tumor xenografts, with 60% of the tumor-bearing mice survived over 100 days.
Increased the percentage of tumor-infiltrating IFN-γ+CD8+ T cells.
Efficiently provoked an adaptive antitumor immune response for tumor regression.
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Animal Model:B16-F10 tumor-bearing mice with radiotherapy[1]
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Dosage:5 mg/kg (D5B is in the form of PCPGd@D5B nanoparticles)
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Administration:Intraperitoneal injection (i.p.); Single dose
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Result:Suppressed 95% of tumor growth, with complete tumor elimination in 43% of the tumor-bearing mice and elongated survival time over 50 days.
Effectively suppressed PD-L1 expression on the surface of tumor cells and TAM membrane.
Promoted the increase of tumor infiltrating CD8+ T cells.
化学情報
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性状 Solid
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分子量 983.15
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分子式 C58H66N2O12
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SMILES
O=C(CCC(N1CC2=CC=CC=C2C#CC3=C1C=CC=C3)=O)OCCOCCOCCOCCOCCOC([C@H]4N(CC5=C(OC)C=C(OCC6=CC=CC(C7=CC=CC=C7)=C6C)C=C5OC)CCCC4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (101.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.54 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.0171 mL | 5.0857 mL | 10.1714 mL | 25.4285 mL |
| 5 mM | 0.2034 mL | 1.0171 mL | 2.0343 mL | 5.0857 mL | |
| 10 mM | 0.1017 mL | 0.5086 mL | 1.0171 mL | 2.5428 mL | |
| 15 mM | 0.0678 mL | 0.3390 mL | 0.6781 mL | 1.6952 mL | |
| 20 mM | 0.0509 mL | 0.2543 mL | 0.5086 mL | 1.2714 mL | |
| 25 mM | 0.0407 mL | 0.2034 mL | 0.4069 mL | 1.0171 mL | |
| 30 mM | 0.0339 mL | 0.1695 mL | 0.3390 mL | 0.8476 mL | |
| 40 mM | 0.0254 mL | 0.1271 mL | 0.2543 mL | 0.6357 mL | |
| 50 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5086 mL | |
| 60 mM | 0.0170 mL | 0.0848 mL | 0.1695 mL | 0.4238 mL | |
| 80 mM | 0.0127 mL | 0.0636 mL | 0.1271 mL | 0.3179 mL | |
| 100 mM | 0.0102 mL | 0.0509 mL | 0.1017 mL | 0.2543 mL |
D5B 関連分類
HY-169392 関連分類
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